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Table 1 Study 1: Pharmacokinetic parameters of riociguat in plasma after a single oral dose of riociguat (pharmacokinetic analysis population, n=29):

From: Bioavailability, pharmacokinetics and safety of riociguat given as an oral suspension or crushed tablet with and without food

Parameter Unit n 2.4 mg high-concentration suspension fasted n 2.4 mg high-concentration suspension fed n 0.3 mg high-concentration suspension fasted n 0.15 mg low-concentration suspension fasted n mgIR tablet fasted
AUC μ*h/L 29 781/49 (230–1515) 29 663/45 (258–1212) 27 91/43 (38–165) 25 47/60 (8.3–91) 29 311/46 (103–587)
AUC/D h/L 29 0.33/49 (0.10–0.63) 29 0.28/45 (0.12–0.50) 27 0.30/43 (0.13–0.55) 25 0.31/60 (0.056–0.61) 29 0.31/46 (0.10–0.59)
Cmax μ/L 29 78/31 (43–128) 29 48/22 (32–70) 29 9.8/33 (4.5–17) 29 4.9/35 (1.9–8.1) 29 36/30 (18–61)
Cmax/D 1/L 29 0.03/31 (0.02–0.05) 29 0.02/22 (0.01–0.29) 29 0.03/33 (0.01–0.06) 29 0.03/35 (0.01–0.05) 29 0.04/30 (0.02–0.06)
tmaxa h 29 1.5 (0.75–4.0) 29 4.0 (3.0–12) 29 1.0 (0.50–3.0) 29 1.0 (0.50–4.0) 29 1.0 (0.50–3.0)
t1/2 h 29 9.2/41 (2.8–21) 29 9.4/33 (4.2–17) 27 7.8/39 (3.5–15) 25 6.8/42 (2.5–12) 29 7.9/43 (3.4–14)
  1. Data presented as geometric mean/% coefficient of variation (range) unless otherwise specified.
  2. a Median (range)
  3. AUC, area under the concentration versus time curve; AUC/D; AUC divided by dose; Cmax, maximum drug concentration in plasma; Cmax/D: Cmax divided by dose; IR, immediate-release; tmax; time to reach Cmax; t1/2; half life